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Drug Delivery Letters

Editor-in-Chief

ISSN (Print): 2210-3031
ISSN (Online): 2210-304X

Research Article

Smart Gn-Keto Nanohybrid Embedded Topical System for Effective Management of Dermatophytosis

Author(s): Nisha Sharma* and Shashikiran Misra

Volume 9, Issue 1, 2019

Page: [21 - 28] Pages: 8

DOI: 10.2174/2210303108666181105112557

Price: $65

Abstract

Background and Objectives: Dermatophytosis (topical fungal infection) is the 4th common disease in the last decade, affecting 20-25% world’s population. Patients of AIDS, cancer, old age senescence, diabetes, cystic fibrosis become more vulnerable to dermatophytosis. The conventional topical dosage proves effective as prophylactic in preliminary stage. In the advanced stage, the therapeutics interacts with healthy tissues before reaching the pathogen site, showing undesirable effects, thus resulting in pitiable patient compliance. The youngest carbon nano-trope “Graphene” is recently used to manipulate bioactive agents for therapeutic purposes. Here, we explore graphene via smart engineering by virtue of high surface area and high payload for therapeutics and developed graphene–ketoconazole nanohybrid (Gn-keto) for potent efficacy towards dermatophytes in a controlled manner.

Methods: Polymethacrylate derivative Eudragit (ERL100 and ERS 100) microspheres embedded with keto and Gn-keto nanohybrid were formulated and characterized through FTIR, TGA, and SEM. In vitro drug release and antifungal activity of formulated Gn-keto microspheres were assessed for controlled release and better efficacy against selected dermatophytes.

Results: Presence of numerous pores within the surface of ERL100 microspheres advocated enhanced solubility and diffusion at the site of action. Controlled diffusion across the dialysis membrane was observed with ERS100 microspheres owing to the nonporous surface and poor permeability. Antifungal activity against T. rubrum and M. canis using microdilution method focused on a preeminent activity (99.785 % growth inhibition) of developed nanohybrid loaded microspheres as compared to 80.876% of keto loaded microspheres for T. rubrum. The culture of M. canis was found to be less susceptible to formulated microspheres.

Conclusion: Synergistic antifungal activity was achieved by nanohybrid Gn-Keto loaded microspheres against selected topical fungal infections suggesting a vital role of graphene towards fungi.

Keywords: Ketoconazole, graphene, nanohybrid, polymethacrylate, antifungal activity, dermatophytosis.

Graphical Abstract
[1]
Kam, N.W.S.; Jessop, T.C.; Wender, P.A.; Dai, H. Nanotube molecular transporters: internalization of carbon nanotube-protein conjugates into mammalian cells. J. Am. Chem. Soc., 2004, 126, 6850-6851.
[2]
Bolotin, K.I.; Sikes, K.J.; Jiang, Z.; Klima, M.; Fudenberg, G.; Hone, J.; Kim, P.; Stormer, H.L. Ultrahigh electron mobility in suspended graphene. Solid State Commun., 2008, 146, 351-355.
[3]
Chen, J.; Peng, H.; Wang, X.; Shao, F.; Yuan, Z.; Han, H. Graphene oxide exhibits broad-spectrum antimicrobial activity against bacterial phytopathogens and fungal conidia by intertwining and membrane perturbation. Nanoscale, 2014, 6, 1879-1889.
[4]
Sundaray, B.; Babu, V.J.; Subramanian, V.; Natarajan, T.S. Preparation and characterization of electrospun fibres of poly(methyl methacrylate) single walled carbon nanotube nanocomposites. J. Eng. Fib. Fab., 2008, 3, 39-45.
[5]
Sawangphruk, M.; Srimuk, P.; Chiochan, P.; Krittayavathananon, A.; Luanwuthi, S.; Limtrakul, J. High-performance supercapacitor of manganese oxide/reduced Graphene oxide nanocomposite coated on flexible carbon fiber paper. Carbon, 2013, 60, 109-116.
[6]
Misra, S.K.; Pandey, H. Carbon Allotrope Graphene: Superstar In Nano World. Int. J. Adv. Pharm., 2013, 2(1), 1-4.
[7]
Pandey, S.; Misra, S.K.; Sharma, N. Synthesis and characterization of graphene-usnic acid conjugate microspheres and its antibacterial activity against Staphylococcus aureus. IJPSR, 2018, 10(2), 1.
[8]
Hellgren, L.; Vincent, J. Lipolytic activity of some dermatophytes. II. Isolation and characterisation of the lipase of Epidermophyton floccosum. J. Med. Microbiol., 1981, 14, 347-350.
[9]
Descamps, F.; Brouta, F.; Baar, D.; Losson, B.; Mignon, B.; Monod, M.; Zaugg, C. Isolation of a Microsporumcanis gene family encoding three Subtilisin like proteases expressed in vivo. J. Invest. Dermatol., 2002, 119, 830-835.
[10]
Duek, L.; Kaufman, G.; Ulman, Y.; Berdicevsky, I. The pathogenesis of dermatophyte infections in human skin sections. J. Infect., 2004, 48, 175-180.
[11]
Rai, S.Y.; Ravikumar, P. Development and evaluation of microsphere based topical formulation using design of experiments. Indian J. Pharm. Sci., 2016, 78, 182-192.
[12]
Woodfolk, J.A. Allergy and Dermatophytes. Clin. Microbiol. Rev., 2005, 18, 30-43.
[13]
Dias, M.F.R.G.; Filho, F.B.; Santos, M.V.P.Q.; Amorim, A.G.F.; Schechtman, R.C.; Azulay, D.R. Treatment of superficial mycoses: Review - part II. An. Bras. Dermatol., 2013, 88, 937-944.
[14]
Das, T.K.; Prusty, S. Graphene-based polymer composites and their applications. Polym. Plast. Technol. Eng., 2013, 52, 319-331.
[15]
Dehghan, S.; Aboofazeli, R.; Avadil, M.; Khaksar, R. Formulation optimization of nifedipine containing microspheres using factorial design. Afr. J. Pharm. Pharmacol., 2010, 4, 346-354.
[16]
Misra, S.K.; Pandey, H.; Patil, S.; Ramteke, P.W.; Pandey, A.C. Tolnaftate loaded polyacrylate electrospun nanofibers for impressive regimen on dermatophytosis. Fibers, 2017, 5, 41-52.
[17]
Wang, X.; Liu, X.; Chen, J.; Han, H.; Yuan, Z. Evaluation and mechanism of antifungal effects of carbon nanomaterials in controlling plant fungal pathogen. Carbon, 2014, 68, 798-806.
[18]
Yang, X.; Zhang, X.; Liu, Z.; Ma, Y.; Huang, Y.; Chen, Y. High-efficiency loading and controlled release of doxorubicin hydrochloride on Graphene oxide. J. Phys. Chem., 2008, 112, 7554-7758.
[19]
Misra, S.K.; Ramteke, P.W.; Patil, S.; Pandey, A.C.; Pandey, H. Tolnaftate- graphene composite loaded nanoengineered electrospun scaffods as efficient therapeutic dressing material for regimen of dermatomycosis. Appl. Nanosci., 2018, 8(7), 1629-1640.

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